PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist

  • Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94. doi: 10.1016/s0960-894x(98)00462-4.
V Ashwood  1 ,  V Brownhill ,  M Higginbottom ,  D C Horwell ,  J Hughes ,  R A Lewthwaite ,  A T McKnight ,  R D Pinnock ,  M C Pritchard ,  N Suman-Chauhan ,  C Webb ,  S C Williams
Affiliations
  • 1. Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, UK.
PMID: 9873586 DOI: 10.1016/s0960-894x(98)00462-4
Abstract

In this paper we describe the development of a novel series of non-peptide, "balanced" neuromedin-B preferring (BB1)/gastrin-releasing peptide preferring (BB2) receptor ligands as exemplified by PD 176252. PD 176252, which exhibits nanomolar affinity for both the BB1 (Ki = 0.15 nM) and BB2 (Ki = 1.0 nM) receptors, has been demonstrated to be a competitive antagonist at these Bombesin Receptor subtypes.

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